AR077055A1 - Derivados de benzimidazol como moduladores del canal trpm8 - Google Patents

Derivados de benzimidazol como moduladores del canal trpm8

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Publication number
AR077055A1
AR077055A1 ARP100102053A ARP100102053A AR077055A1 AR 077055 A1 AR077055 A1 AR 077055A1 AR P100102053 A ARP100102053 A AR P100102053A AR P100102053 A ARP100102053 A AR P100102053A AR 077055 A1 AR077055 A1 AR 077055A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
group
heterocycloalkyl
heteroaryl
cycloalkyl
Prior art date
Application number
ARP100102053A
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English (en)
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Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR077055A1 publication Critical patent/AR077055A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se describen los compuestos, composiciones y métodos para tratar diferentes enfermedades, síndromes, afecciones y trastornos que incluyen el dolor. Reivindicacion 1: Un compuesto de la formula (1) en donde a es un numero entero de 0 a 3; cada R0 se selecciona independientemente del grupo que consiste de halogeno, hidroxi, ciano, alquilo inferior, alquilo inferior fluorado, alcoxi inferior y alcoxi inferior fluorado; R2 se selecciona del grupo que consiste de hidrogeno, halogeno, hidroxi, ciano, alquilo inferior, alquilo inferior fluorado, alcoxi inferior y alcoxi inferior fluorado; R1 se selecciona del grupo que consiste de alquilo, alquilo inferior sustituido con hidroxi, alquilo inferior halogenado, cicloalquilo-(alquilo inferior) y fenilo-(alquilo inferior); alternativamente, R2 y R1 se toman juntos como en restos (2) o (3); R3 se selecciona del grupo que consiste de alquilo inferior, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilo-(alquilo inferior), arilo-(alquilo inferior), heteroarilo-(alquilo inferior) y heterocicloalquilo-(alquilo inferior); en donde el cicloalquilo, arilo, heteroarilo o heterocicloalquilo, ya sea solo o como parte de un grupo sustituyente se sustituye opcionalmente con uno o más sustituyentes independientemente seleccionados del grupo que consiste de halogeno, alquilo inferior, alquilo inferior halogenado, alcoxi inferior, alcoxi inferior halogenado, -C(O)OH, -C(O)O-(alquilo inferior) y -C(O)NRARB; en donde RA y RB se seleccionan independientemente del grupo que consiste de hidrogeno y alquilo inferior; alternativamente RA y RB se toman juntos con el átomo de nitrogeno al cual están unidos para formar una estructura de anillo que contiene nitrogeno saturado de 5 a 6 miembros; R4 se selecciona del grupo que consiste de alquilo inferior, cicloalquilo, arilo, heteroarilo, heterocicloalquilo, cicloalquilo-(alquilo inferior), arilo-(alquilo inferior), heteroarilo-(alquilo inferior) y heterocicloalquilo-(alquilo inferior); en donde el cicloalquilo, arilo, heteroarilo o heterocicloalquilo, ya sea solo o como parte de un grupo sustituyente se sustituye opcionalmente con uno o más sustituyentes independientemente seleccionados del grupo que consiste de halogeno, alquilo inferior, alquilo inferior halogenado, alcoxi inferior, alcoxi inferior halogenado y -S-CF3; siempre y cuando R4 sea heteroarilo o heterocicloalquilo, entonces el grupo R4 está unido al N del compuesto de la formula (1) a través de un átomo de carbono; o una sal farmacéuticamente aceptable de éstos.
ARP100102053A 2009-06-10 2010-06-10 Derivados de benzimidazol como moduladores del canal trpm8 AR077055A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US18568609P 2009-06-10 2009-06-10

Publications (1)

Publication Number Publication Date
AR077055A1 true AR077055A1 (es) 2011-07-27

Family

ID=42670634

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102053A AR077055A1 (es) 2009-06-10 2010-06-10 Derivados de benzimidazol como moduladores del canal trpm8

Country Status (11)

Country Link
US (1) US8242157B2 (es)
EP (1) EP2440294B1 (es)
JP (1) JP2012530053A (es)
CN (1) CN102802731A (es)
AR (1) AR077055A1 (es)
AU (1) AU2010258714B2 (es)
CA (1) CA2764567A1 (es)
HK (1) HK1169070A1 (es)
RU (1) RU2011153431A (es)
TW (1) TW201103941A (es)
WO (1) WO2010144680A1 (es)

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CA2412215A1 (en) * 2000-06-16 2001-12-27 Curis, Inc. Angiogenesis-modulating compositions and uses
CN103354812A (zh) 2010-12-09 2013-10-16 詹森药业有限公司 作为trpm8调节剂的咪唑并[1,2-a]吡啶磺酰胺
WO2012098281A2 (es) 2011-01-19 2012-07-26 Universidad Miguel Hernández De Elche Péptidos moduladores de receptores trp y sus usos
PL2686302T3 (pl) 2011-03-16 2017-01-31 Mitsubishi Tanabe Pharma Corporation Związki sulfonamidowe mające działanie antagonistyczne dla TRPMS
JP2014527511A (ja) * 2011-06-24 2014-10-16 アムジエン・インコーポレーテツド Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用
JP5985453B2 (ja) * 2012-09-14 2016-09-06 田辺三菱製薬株式会社 医薬組成物
WO2014042238A1 (ja) 2012-09-14 2014-03-20 田辺三菱製薬株式会社 スルホンアミド化合物
UA119848C2 (uk) 2013-03-15 2019-08-27 Інсайт Холдинґс Корпорейшн Трициклічні гетероцикли як інгібітори білків бет
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EA039678B1 (ru) 2014-04-23 2022-02-24 Инсайт Корпорейшн 1H-ПИРРОЛО[2,3-c]ПИРИДИН-7(6H)-ОНЫ И ПИРАЗОЛО[3,4-c]ПИРИДИН-7(6H)-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕЛКОВ BET
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為ｂｅｔ蛋白抑制劑之三環雜環
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
US10993939B2 (en) 2016-06-13 2021-05-04 Mitsubishi Tanabe Pharmaceutical Company Compositions for treating or preventing vasomotor symptoms
PT3472157T (pt) 2016-06-20 2023-05-30 Incyte Corp Formas sólidas cristalinas de um inibidor bet
WO2020038387A1 (zh) * 2018-08-24 2020-02-27 杭州阿诺生物医药科技有限公司 高活性sting蛋白激动剂
CN112608331B (zh) * 2018-08-29 2022-03-11 杭州阿诺生物医药科技有限公司 中间体及其在合成sting蛋白激动剂化合物中的应用
WO2020132566A1 (en) * 2018-12-21 2020-06-25 Nimbus Titan, Inc. Sting pyrazole agonists and uses thereof
WO2020151682A1 (zh) * 2019-01-23 2020-07-30 成都先导药物开发股份有限公司 一种大环类免疫调节剂
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2651865C (en) * 2006-05-10 2015-11-24 Janssen Pharmaceutica N.V. Cold menthol receptor-1 antagonists
US20080287398A1 (en) * 2007-05-02 2008-11-20 Colburn Raymond W Cold menthol receptor-1 antagonists
WO2009012430A1 (en) * 2007-07-18 2009-01-22 Janssen Pharmaceutica N.V. Sulfonamides as trpm8 modulators

Also Published As

Publication number Publication date
CA2764567A1 (en) 2010-12-16
CN102802731A (zh) 2012-11-28
AU2010258714A1 (en) 2012-01-12
TW201103941A (en) 2011-02-01
HK1169070A1 (en) 2013-01-18
EP2440294B1 (en) 2013-07-24
WO2010144680A1 (en) 2010-12-16
EP2440294A1 (en) 2012-04-18
US8242157B2 (en) 2012-08-14
US20110003801A1 (en) 2011-01-06
JP2012530053A (ja) 2012-11-29
AU2010258714B2 (en) 2014-09-11
RU2011153431A (ru) 2013-07-20

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